Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders

SRC: A Century of Science Brought to the Clinic

(2015) Alexey Aleshin et al.   NEOPLASIA

Dual Functions of Bruton's Tyrosine Kinase and Tec Kinase during Fc  Receptor-Induced Signaling and Phagocytosis

(2014) J. Jongstra-Bilen et al.   JOURNAL OF IMMUNOLOGY

In vitro and in vivo chemosensitizing activity of LFM-A13, a dual-function inhibitor of Bruton's tyrosine kinase and polo-like kinases, against human leukemic B-cell precursors

(2011) Fatih Uckun et al.   ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH

An important role for Akt3 in platelet activation and thrombosis

(2011) K. A. O'Brien et al.   BLOOD

SYK inhibition and response prediction in diffuse large B-cell lymphoma

(2011) S. Cheng et al.   BLOOD

Safety and efficacy of bosutinib (SKI-606) in chronic phase Philadelphia chromosome-positive chronic myeloid leukemia patients with resistance or intolerance to imatinib

(2011) J. E. Cortes et al.   BLOOD

Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765

(2011) S. E. M. Herman et al.   BLOOD

The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo

(2011) S. Ponader et al.   BLOOD

KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancer

(2011) Muralidharan Anbalagan et al.   BREAST CANCER RESEARCH AND TREATMENT

Inducing apoptosis in chemotherapy-resistant B-lineage acute lymphoblastic leukaemia cells by targeting HSPA5, a master regulator of the anti-apoptotic unfolded protein response signalling network

(2011) Fatih M. Uckun et al.   BRITISH JOURNAL OF HAEMATOLOGY

Phase II Study of Dasatinib in Relapsed or Refractory Chronic Lymphocytic Leukemia

(2011) P. C. Amrein et al.   CLINICAL CANCER RESEARCH

2.23 Covalent Inhibition of Btk with Clinical Development Compound AVL-292 Disrupts Signaling That Maintains the Microenvironment Necessary for Chronic Lymphocytic Leukemia Growth

(2011) E. Evans et al.   Clinical Lymphoma Myeloma & Leukemia

The Src Family Kinase Inhibitors PP2 and PP1 Block TGF-Beta1-Mediated Cellular Responses by Direct and Differential Inhibition of Type I and Type II TGF-Beta Receptors

(2011) H. Ungefroren et al.   CURRENT CANCER DRUG TARGETS

Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase Inhibitor

(2011) L. Liu et al.   DRUG METABOLISM AND DISPOSITION

Antiarthritis Effect of a Novel Bruton's Tyrosine Kinase (BTK) Inhibitor in Rat Collagen-Induced Arthritis and Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling: Relationships between Inhibition of BTK Phosphorylation and Efficacy

(2011) L. Liu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

The Bruton tyrosine kinase inhibitor PCI-32765 ameliorates autoimmune arthritis by inhibition of multiple effector cells

(2011) Betty Y Chang et al.   ARTHRITIS RESEARCH & THERAPY

An oral Syk kinase inhibitor in the treatment of rheumatoid arthritis: A three-month randomized, placebo-controlled, phase II study in patients with active rheumatoid arthritis that did not respond to biologic agents

(2010) Mark C. Genovese et al.   ARTHRITIS AND RHEUMATISM

The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the E - TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling

(2010) M. Suljagic et al.   BLOOD

Angiopoietin-2 in CLL

(2010) J. A. Burger   BLOOD

The novel receptor tyrosine kinase Axl is constitutively active in B-cell chronic lymphocytic leukemia and acts as a docking site of nonreceptor kinases: implications for therapy

(2010) A. K. Ghosh et al.   BLOOD

Targeting SYK kinase-dependent anti-apoptotic resistance pathway in B-lineage acute lymphoblastic leukaemia (ALL) cells with a potent SYK inhibitory pentapeptide mimic

(2010) Fatih M. Uckun et al.   BRITISH JOURNAL OF HAEMATOLOGY

A phase I study of imatinib mesylate in combination with chlorambucil in previously treated chronic lymphocytic leukemia patients

(2010) Jonathan Hebb et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Phase I Safety, Pharmacokinetics, and Inhibition of Src Activity Study of Saracatinib in Patients with Solid Tumors

(2010) J. Baselga et al.   CLINICAL CANCER RESEARCH

Metabolism of Fostamatinib, the Oral Methylene Phosphate Prodrug of the Spleen Tyrosine Kinase Inhibitor R406 in Humans: Contribution of Hepatic and Gut Bacterial Processes to the Overall Biotransformation

(2010) D. J. Sweeny et al.   DRUG METABOLISM AND DISPOSITION

Membrane-associated signaling in human B-lymphoma lines

(2010) Sebastien Tauzin et al.   EXPERIMENTAL CELL RESEARCH

Bruton's tyrosine kinase as a molecular target in treatment of leukemias and lymphomas as well as inflammatory disorders and autoimmunity

(2010) Fatih M Uckun et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Spleen tyrosine kinase as a molecular target for treatment of leukemias and lymphomas

(2010) Fatih M Uckun et al.   Expert Review of Anticancer Therapy

Human remyelination promoting antibody inhibits apoptotic signaling and differentiation through Lyn kinase in primary rat oligodendrocytes

(2010) J. Watzlawik et al.   GLIA

Safety, Pharmacokinetics, and Preliminary Clinical Activity of Inotuzumab Ozogamicin, a Novel Immunoconjugate for the Treatment of B-Cell Non-Hodgkin's Lymphoma: Results of a Phase I Study

(2010) Anjali Advani et al.   JOURNAL OF CLINICAL ONCOLOGY

Anomalous constitutive Src kinase activity promotes B lymphoma survival and growth

(2010) Jiyuan Ke et al.   Molecular Cancer

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

(2010) R. Eric Davis et al.   NATURE

An Oral Spleen Tyrosine Kinase (Syk) Inhibitor for Rheumatoid Arthritis

(2010) Michael E. Weinblatt et al.   NEW ENGLAND JOURNAL OF MEDICINE

STAT3 is a substrate of SYK tyrosine kinase in B-lineage leukemia/lymphoma cells exposed to oxidative stress

(2010) F. M. Uckun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Augmentation of the Antileukemia Potency of Total-Body Irradiation (TBI) by a Novel P-site Inhibitor of Spleen Tyrosine Kinase (SYK)

(2010) F. M. Uckun et al.   RADIATION RESEARCH

Contribution of gut bacteria to the metabolism of the spleen tyrosine kinase (Syk) inhibitor R406 in cynomolgus monkey

(2010) D. J. Sweeny et al.   XENOBIOTICA

A Computational Approach to Analyze the Mechanism of Action of the Kinase Inhibitor Bafetinib

(2010) Thomas R. Burkard et al.   PLoS Computational Biology

Primary B Cell Immunodeficiencies: Comparisons and Contrasts

(2009) Mary Ellen Conley et al.   Annual Review of Immunology

Syk and pTyr'd: Signaling through the B cell antigen receptor

(2009) Robert L. Geahlen   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

B-cell antigen receptor signaling enhances chronic lymphocytic leukemia cell migration and survival: specific targeting with a novel spleen tyrosine kinase inhibitor, R406

(2009) M. P. Quiroga et al.   BLOOD

Inhibition of Syk with fostamatinib disodium has significant clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia

(2009) J. W. Friedberg et al.   BLOOD

Spleen Tyrosine Kinase Is Overexpressed and Represents a Potential Therapeutic Target in Chronic Lymphocytic Leukemia

(2009) Maike Buchner et al.   CANCER RESEARCH

Structural Insights for Design of Potent Spleen Tyrosine Kinase Inhibitors from Crystallographic Analysis of Three Inhibitor Complexes

(2009) Armando G. Villaseñor et al.   Chemical Biology & Drug Design

Src Tyrosine Kinase Regulates Adhesion and Chemotaxis in Waldenstrom Macroglobulinemia

(2009) H. T. Ngo et al.   CLINICAL CANCER RESEARCH

Bruton's tyrosine kinase as a drug discovery target

(2009) Z. Pan   DRUG NEWS & PERSPECTIVES

A novel Syk kinase inhibitor suitable for inhalation: R-343(?) – WO-2009031011

(2009) Peter Norman   EXPERT OPINION ON THERAPEUTIC PATENTS

Therapeutic prospect of Syk inhibitors

(2009) Paolo Ruzza et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Multiple roles of Lyn kinase in myeloid cell signaling and function

(2009) Patrizia Scapini et al.   IMMUNOLOGICAL REVIEWS

Bruton’s tyrosine kinase (Btk): function, regulation, and transformation with special emphasis on the PH domain

(2009) Abdalla J. Mohamed et al.   IMMUNOLOGICAL REVIEWS

A Spleen Tyrosine Kinase Inhibitor Reduces the Severity of Established Glomerulonephritis

(2009) J. Smith et al.   JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY

Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530

(2009) Tim P. Green et al.   Molecular Oncology

The tyrosine kinase Syk regulates the survival of chronic lymphocytic leukemia B cells through PKCδ and proteasome-dependent regulation of Mcl-1 expression

(2009) A D Baudot et al.   ONCOGENE

The Difference in Biological Properties between Parental and v-Ha-ras Transformed NIH3T3 Cells

(2009) Michael Lee et al.   Cancer Research and Treatment

Inhibition of Protein Kinase c-Src as a Therapeutic Approach for Cancer and Bone Metastases

(2008) Nadia Rucci et al.   Anti-Cancer Agents in Medicinal Chemistry

Treatment of rheumatoid arthritis with a syk kinase inhibitor: A twelve-week, randomized, placebo-controlled trial

(2008) Michael E. Weinblatt et al.   ARTHRITIS AND RHEUMATISM

An orally bioavailable spleen tyrosine kinase inhibitor delays disease progression and prolongs survival in murine lupus

(2008) Frances Rena Bahjat et al.   ARTHRITIS AND RHEUMATISM

Of mice and men: an open-label pilot study for treatment of immune thrombocytopenic purpura by an inhibitor of Syk

(2008) A. Podolanczuk et al.   BLOOD

The kinase inhibitor dasatinib induces apoptosis in chronic lymphocytic leukemia cells in vitro with preference for a subgroup of patients with unmutated IgVH genes

(2008) A. Veldurthy et al.   BLOOD

Dasatinib sensitizes primary chronic lymphocytic leukaemia lymphocytes to chlorambucil and fludarabinein vitro

(2008) Lilian Amrein et al.   BRITISH JOURNAL OF HAEMATOLOGY

Overcoming imatinib resistance using Src inhibitor CGP76030, Abl inhibitor nilotinib and Abl/Lyn inhibitor INNO-406 in newly established K562 variants withBCR-ABLgene amplification

(2008) Koji Morinaga et al.   INTERNATIONAL JOURNAL OF CANCER

PSGL-1 engagement by E-selectin signals through Src kinase Fgr and ITAM adapters DAP12 and FcRγ to induce slow leukocyte rolling

(2008) Alexander Zarbock et al.   JOURNAL OF EXPERIMENTAL MEDICINE